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Cepharanthine, a bisbenzylisoquinoline alkaloid, inhibits lipopolysaccharide-induced microglial activation.

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Activation of microglial cells in the brain has been considered to be associated with various neurodegenerative diseases (NDD). In this study, cepharanthine, a bisbenzylisoquinoline alkaloid, was found to inhibit lipopolysaccharide… Click to show full abstract

Activation of microglial cells in the brain has been considered to be associated with various neurodegenerative diseases (NDD). In this study, cepharanthine, a bisbenzylisoquinoline alkaloid, was found to inhibit lipopolysaccharide (LPS)-induced microglial activation. Cepharanthine suppressed the release of nitric oxide (NO) by LPS-activated primary mouse cortical microglia and/or BV2 microglial cell line. Cepharanthine reduced LPS-induced mRNA expression of inducible NO synthase (iNOS), but it did not display direct NO-scavenging activity up to 100 μM in sodium nitroprusside (SNP) solution. Further studies revealed that cepharanthine suppressed the release of cytokines (TNF-α, IL-1β, and IL-6) by LPS-activated microglial cells. Cepharanthine may have potential in the treatment of neurodegenerative diseases accompanied by microglial activation.

Keywords: bisbenzylisoquinoline alkaloid; induced microglial; cepharanthine; cepharanthine bisbenzylisoquinoline; activation; microglial activation

Journal Title: Die Pharmazie
Year Published: 2019

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